Assay Detail
Binding
CHEMBL5046488
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [3H]-N-methylspiperone from human dopamine D3 receptor expressed in HEK293 cell membranes incubated for 60 mins by microbeta scintillation counting analysis
46
Total Activities
46
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Novel Dual-Target μ-Opioid Receptor and Dopamine D<sub>3</sub> Receptor Ligands as Potential Nonaddictive Pharmacotherapeutics for Pain Management.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 46 | 6.17 | 8.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5081136 | — | — | 1 | 8.66 |
| CHEMBL54 | HALOPERIDOL | 4.0 | 1 | 8.36 |
| CHEMBL5093200 | — | — | 1 | 7.93 |
| CHEMBL5074399 | — | — | 1 | 7.75 |
| CHEMBL5073754 | — | — | 1 | 7.41 |
| CHEMBL5088070 | — | — | 1 | 7.16 |
| CHEMBL5092243 | — | — | 1 | 7.03 |
| CHEMBL5071238 | — | — | 1 | 6.91 |
| CHEMBL5089655 | — | — | 1 | 6.88 |
| CHEMBL5075990 | — | — | 1 | 6.87 |
| CHEMBL5085974 | — | — | 1 | 6.77 |
| CHEMBL5083441 | — | — | 1 | 6.70 |
| CHEMBL5083473 | — | — | 1 | 6.63 |
| CHEMBL5087504 | — | — | 1 | 6.60 |
| CHEMBL5089932 | — | — | 1 | 6.58 |
| CHEMBL5079053 | — | — | 1 | 6.54 |
| CHEMBL5076359 | — | — | 1 | 6.47 |
| CHEMBL5073904 | — | — | 1 | 6.34 |
| CHEMBL5087543 | — | — | 1 | 6.24 |
| CHEMBL5090215 | — | — | 1 | 5.97 |
| CHEMBL5077114 | — | — | 1 | 5.89 |
| CHEMBL5077104 | — | — | 1 | 5.87 |
| CHEMBL5091656 | — | — | 1 | 5.81 |
| CHEMBL5075726 | — | — | 1 | 5.80 |
| CHEMBL5084145 | — | — | 1 | 5.79 |
| CHEMBL5080654 | — | — | 1 | 5.76 |
| CHEMBL841 | LOPERAMIDE | 4.0 | 1 | 5.71 |
| CHEMBL5070377 | — | — | 1 | 5.68 |
| CHEMBL651 | METHADONE | 4.0 | 1 | 5.68 |
| CHEMBL5079903 | — | — | 1 | 5.65 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5081136 | — | Ki | = | 2.21 | nM | 8.66 |
| CHEMBL54 | HALOPERIDOL | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL5093200 | — | Ki | = | 11.8 | nM | 7.93 |
| CHEMBL5074399 | — | Ki | = | 17.8 | nM | 7.75 |
| CHEMBL5073754 | — | Ki | = | 39.2 | nM | 7.41 |
| CHEMBL5088070 | — | Ki | = | 69.0 | nM | 7.16 |
| CHEMBL5092243 | — | Ki | = | 93.8 | nM | 7.03 |
| CHEMBL5071238 | — | Ki | = | 123.0 | nM | 6.91 |
| CHEMBL5089655 | — | Ki | = | 132.0 | nM | 6.88 |
| CHEMBL5075990 | — | Ki | = | 135.0 | nM | 6.87 |
| CHEMBL5085974 | — | Ki | = | 171.0 | nM | 6.77 |
| CHEMBL5083441 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL5083473 | — | Ki | = | 235.0 | nM | 6.63 |
| CHEMBL5087504 | — | Ki | = | 249.0 | nM | 6.60 |
| CHEMBL5089932 | — | Ki | = | 260.0 | nM | 6.58 |
| CHEMBL5079053 | — | Ki | = | 288.0 | nM | 6.54 |
| CHEMBL5076359 | — | Ki | = | 342.0 | nM | 6.47 |
| CHEMBL5073904 | — | Ki | = | 460.0 | nM | 6.34 |
| CHEMBL5087543 | — | Ki | = | 572.0 | nM | 6.24 |
| CHEMBL5090215 | — | Ki | = | 1060.0 | nM | 5.97 |
| CHEMBL5077114 | — | Ki | = | 1290.0 | nM | 5.89 |
| CHEMBL5077104 | — | Ki | = | 1360.0 | nM | 5.87 |
| CHEMBL5091656 | — | Ki | = | 1550.0 | nM | 5.81 |
| CHEMBL5075726 | — | Ki | = | 1600.0 | nM | 5.80 |
| CHEMBL5084145 | — | Ki | = | 1630.0 | nM | 5.79 |
| CHEMBL5080654 | — | Ki | = | 1720.0 | nM | 5.76 |
| CHEMBL841 | LOPERAMIDE | Ki | = | 1940.0 | nM | 5.71 |
| CHEMBL5070377 | — | Ki | = | 2080.0 | nM | 5.68 |
| CHEMBL651 | METHADONE | Ki | = | 2110.0 | nM | 5.68 |
| CHEMBL5079903 | — | Ki | = | 2240.0 | nM | 5.65 |
| CHEMBL5086564 | — | Ki | = | 2300.0 | nM | 5.64 |
| CHEMBL5072449 | — | Ki | = | 3810.0 | nM | 5.42 |
| CHEMBL346331 | NORMETHADONE | Ki | = | 4270.0 | nM | 5.37 |
| CHEMBL5083186 | — | Ki | = | 4350.0 | nM | 5.36 |
| CHEMBL5075014 | — | Ki | = | 5630.0 | nM | 5.25 |
| CHEMBL5090346 | — | Ki | = | 8960.0 | nM | 5.05 |
| CHEMBL5082465 | — | Ki | = | 13700.0 | nM | 4.86 |
| CHEMBL5077645 | — | Ki | = | 15700.0 | nM | 4.80 |
| CHEMBL346898 | — | Ki | = | 16100.0 | nM | 4.79 |
| CHEMBL596 | FENTANYL | Ki | = | 26200.0 | nM | 4.58 |
| CHEMBL5094044 | — | Ki | = | 36900.0 | nM | 4.43 |
| CHEMBL5087408 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5091775 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5091335 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5094927 | — | Ki | > | 100000.0 | nM | - |
| CHEMBL5091479 | — | Ki | > | 100000.0 | nM | - |